Isolation Of Water Soluble Constituents From Arnebia Euchroma And Study On Compound Granules

Objectives: We studied the water soluble constituents of roots from Arnebia euchroma on the basis of the previous study and optimized the water extraction and alcohol sedimentation and the preparing technology based on the activity of HIV-1 IN (HIV-1 integrase) in vitro. Methods:â‘ The water soluble constituents were isolated by conventional methods and different kinds of column chromatography. The structures were elucidated by chemical and spectroscopic analysis.â‘¡we evaluated and optimumed the technology of water extraction and alcohol-precipitation by the contents of caffeic acid tetramer and salvianolic Acid B.â‘¢HIV-1 IN and HIV-1 PR and HIV-1RT were used to screen the activity of the samples in vitro.â‘£The composition of the formulation and the amounts of the excipients on granules were sieved by the synthesizing multiple guidelines method. Results:â‘ We isolated three water soluble constituents from Arnebia euchroma and the structures were identified as 2-(4'-hydroxy-3'-methoxy-phenl) -3-hydroxymethyl-6-methoxy-2, 3-dihydro-benzofuran-5-carboxylic acid( I) , caffeic acid tetramer (II), and isomer of caffeic acid tetramer (III) respectively.â‘¡It was found that the best technology is : 16 times of water, extraction 3 times, each times for 1 hour, 70% alcohol used for sedimentation, material/extraction solution ratio of 1:2(g/ml).The concents of caffic acid tetramer and salvianolic Acid B in original formulation was 3.84mg/g, 19.59mg/g, respectively.â‘¢The optimum formulation for granule was 1 portion of extract to 1. 5 portion saccharum lactis. 6 samples showed the inhibitionactivity to HIV-1 IN invitro, especially the first sample. Conclusions:â‘ Caffeic acid tetramer and its isomer are the main water soluble constituents of Arnebia euchroma and caffic acid tetramer shows the strong inhibition activity on HIV-1 IN .â‘¡Purity of caffeic acid tetramer reached the standard of the chemical reference in Chinese medicinal herbs.â‘¢Verification test manifested that the extraction conditions were stable and feasible.â‘£The optimum granules showed good solubility and low hydroscopicity and high briquetting.